1. Membrane Transporter/Ion Channel
  2. EAAT2
  3. LDN-212320

LDN-212320 (Synonyms: LDN/OSU-0212320; LDN-0212320; OSU-0212320)

Cat. No.: HY-12741 Purity: 96.72%
Handling Instructions

LDN-212320(OSU-0212320) is a glutamate transporter EAAT2 activator; enhances EAAT2 levels by > 6 fold at concentrations < 5 μM after 24 h.

For research use only. We do not sell to patients.

LDN-212320 Chemical Structure

LDN-212320 Chemical Structure

CAS No. : 894002-50-7

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10 mM * 1 mL in DMSO USD 134 In-stock
Estimated Time of Arrival: December 31
10 mg USD 122 In-stock
Estimated Time of Arrival: December 31
50 mg USD 456 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

LDN-212320(OSU-0212320) is a glutamate transporter EAAT2 activator; enhances EAAT2 levels by > 6 fold at concentrations < 5 μM after 24 h. IC50 value: 1.83 uM(EC50) [2] Target: EAAT2 activator in vitro: LDN/OSU-0212320 increased EAAT2 protein levels in a dose-dependent(EC50=1.83 ± 0.27 μM) and time-dependent manner. LDN/OSU-0212320 increased EAAT2 protein levels and glutamate uptake function, but did not affect EAAT1 or EAAT3 protein levels. LDN/OSU-0212320 treatment markedly prevented neuronal loss and degeneration, as assessed by MAP2 immunostaining [2]. in vivo: After a single i.p. 40-mg/kg dose of LDN/OSU-0212320, EAAT2 protein levels and associated glutamate uptake increased by approximately 1.5- to 2-fold at 2 hours and by approximately 2- to 3-fold between 8 and 24 hours after injection. Even 72 hours after injection, an approximately 1.5-fold increase in EAAT2 protein levels could still be detected (data not shown). In addition, we found that LDN/OSU-0212320–induced EAAT2 protein levels and glutamate uptake were dose dependent [2]. Small-molecule activator of glutamate transporter EAAT2 translation provides neuroprotection By Kong, Qiongman; Chang, Ling-Chu; Takahashi, Kou; Liu, Qibing; Schulte, Delanie A.; Lai, Liching; Ibabao, Brian; Lin, Yuchen; Stouffer, Nathan; Das Mukhopadhyay, Chitra; et al From Journal of Clinical Investigation (2014), 124(3), 1255-1267. Structure-activity relationship study of pyridazine derivatives as glutamate transporter EAAT2 activators By Xing, Xuechao; Chang, Ling-Chu; Kong, Qiongman; Colton, Craig K.; Lai, Liching; Glicksman, Marcie A.; Lin, Chien-Liang Glenn; Cuny, Gregory D. From Bioorganic & Medicinal Chemistry Letters (2011), 21(19), 5774-5777.

Molecular Weight

293.39

Formula

C₁₇H₁₅N₃S

CAS No.

894002-50-7

SMILES

CC1=CC=CC=C1CSC2=NN=C(C3=NC=CC=C3)C=C2

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (170.42 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.4084 mL 17.0422 mL 34.0843 mL
5 mM 0.6817 mL 3.4084 mL 6.8169 mL
10 mM 0.3408 mL 1.7042 mL 3.4084 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (8.52 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (8.52 mM); Clear solution

*All of the co-solvents are provided by MCE.
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LDN-212320
Cat. No.:
HY-12741
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